Acetylsalicylic acid - instructions for use, dose, side effects, contraindications

Description:Tablets of white color, slightly marble, flat-cylindrical shape with a facet and a risk without a smell or with a weak characteristic odor.

Pharmacotherapeutic group:Non-steroidal anti-inflammatory drug (NSAID)

ATX: & nbsp

N.02.B.A Salicylic acid and its derivatives

Pharmacodynamics:

The drug has analgesic, antipyretic, anti-inflammatory effect, which is due to the inhibition of cyclooxygenases involved in the synthesis prostaglandins. Acetylsalicylic acid inhibits platelet aggregation by blocking the synthesis of thromboxane A₂.

Pharmacokinetics:

At intake the absorption is complete. During absorption, it undergoes presystemic elimination in the intestinal wall and in the liver (deacetylated).The absorbed part is quickly hydrolyzed by nonspecific cholinesterases of plasma and albumin esterase, therefore the elimination half-life is no more than 15-20 minutes.

In the body it circulates (75-90% in association with albumin) and is distributed in tissues as an anion of salicylic acid.

Time to reach a maximum concentration of 2 hours. The serum concentration of salicylates is very variable. Salicylates easily penetrate into many tissues and body fluids, including spinal, peritoneal and synovial fluid. Penetration into the joint cavity is accelerated in the presence of hyperemia and edema and slows down in the proliferative phase of inflammation. In small amounts, salicylates are found in the nervous tissue, traces in bile, sweat, feces. When acidosis occurs, most of the salicylic acid is converted to a non-ionized acid that penetrates well into the tissue, including the brain. Rapidly passes through the placenta, in small quantities is excreted in breast milk.

Metabolized mainly in the liver with the formation of 4 metabolites, found in many tissues and urine.

It is excreted mainly by active secretion in the renal tubules in the form of salicylic acid (60%) and in the form of metabolites.Elimination of salicylic acid depends on the pH of the urine (urine alkalinization increases the ionization of salicylates, their reabsorption worsens and the excretion increases significantly). The rate of excretion depends on the dose: when taking small doses, the half-life period is 2-3 hours, with an increase in the dose it can increase to 15-30 hours.

Indications:

Treatment of moderate or mild pain syndrome: headache (including associated with alcohol withdrawal syndrome), toothache, migraine, sore throat, back and muscle pain, joint pain, neuralgia, radicular syndrome, algodismenorrhea (menstruation pain) .

Feverish syndrome with colds and other infectious and inflammatory diseases in adults and children over 15 years of age.

Contraindications:

- Children up to 15 years of age;

- hypersensitivity to acetylsalicylic acid, other non-steroidal anti-inflammatory drugs and components of the drug;

- deficiency of glucose-6-phosphate dehydrogenase;

- complete or incomplete combination of bronchial asthma, recurrent polyposis mucous membrane of the nose and paranasal sinuses and intolerance of ASA, etc. NSAIDs (including in the anamnesis);

- Pregnancy (I and III trimester), the period of breastfeeding;

- erosive-ulcerative lesions of the gastrointestinal tract (in the phase of exacerbation), gastrointestinal bleeding;

- hemorrhagic diathesis (hemophilia, von Willebrand's disease, telangiectasia, hypoprothrombinemia, thrombocytopenic purpura);

- severe hepatic impairment or active liver disease;

- exacerbation of inflammatory bowel diseases (ulcerative colitis, disease Crown);

- cerebrovascular bleeding or other bleeding;

- deficiency of vitamin K;

- simultaneous administration with methotrexate in a dose of 15 mg / day or more;

- simultaneous administration of oral anticoagulants and acetylsalicylic acid in a dose exceeding 3 g per day;

- marked renal failure (creatinine clearance less than 30 ml / min).

Carefully:

Hyperuricemia, urate nephrolithiasis, gout, peptic ulcer and / or duodenal ulcers or gastrointestinal hemorrhage (history), renal failure (creatinine clearance 30-60 ml / min), liver failure, bronchial asthma, chronic obstructive pulmonary disease, polyposis nose, hay fever,drug allergy, pregnancy (II trimester), simultaneous reception of anticoagulants and acetylsalicylic acid in a dose of less than 3 g per day, simultaneous reception of methotrexate in a dose of less than 15 mg / day, metrorrhagia (acyclic uterine bleeding), hypermenorrhea (profuse and prolonged menstruation).

Pregnancy and lactation:

A drug Acetylsalicylic acid contraindicated in the first and third trimester of pregnancy. Use in the second trimester of pregnancy - with caution, only if the potential use of the application exceeds the potential risk to the fetus. It is necessary to consult a doctor.

During breastfeeding, taking the drug is contraindicated.

Dosing and Administration:

Inside, after eating, washed down with water or alkaline mineral water.

Adults and children over 15 years of age: a single dose of 500 mg, a maximum single dose of 1000 mg (2 tablets of 500 mg), a maximum daily dose of 3000 g (6 tablets of 500 mg). A single dose, if necessary, can be taken 3-4 times a day with an interval of at least 4 hours.

The duration of treatment (without consulting a doctor) should not exceed 5 days with an appointment as an anesthetic and more than 3 days - as an antipyretic.

To reduce the risk of developing adverse events from the gastrointestinal tract (GIT), a minimum effective dose should be used with the minimum possible short course.

Side effects:

The adverse events presented below are listed according to anatomophysiological classification and frequency of occurrence. The frequency of occurrence is determined by WHO and has the following gradation: often - more than 1%; infrequently, 0.1-1%; rarely - 0,01 - 0,1%; very rarely - less than 0.01%, including individual cases.

From the gastrointestinal tract: often - nausea, vomiting, pain in the epigastric region, decreased appetite, rarely - diarrhea (diarrhea), gastrointestinal bleeding (vomiting like "coffee grounds", black "tarry" stool); very rarely - increased activity of "liver" transaminases, in some cases - ulcer - perforation of the stomach.

From the nervous system: infrequently - headache, dizziness, in some cases - reduced severity of hearing, ringing in the ears.

From the side of the blood and lymphatic system: infrequently - hemorrhagic syndrome (epistaxis, bleeding gums, hemorrhagic rash), increase in clotting time. These effects persist for 4-8 days with the moment of discontinuation of the drug and should be taken into account in planning subsequent operations for patients.

From the immune system: often - skin rash, very rarely - bronchospasm, angioedema. Formation on the basis of the hapten mechanism of the "aspirin" triad (combination of bronchial asthma, recurrent polyposis of nose and paranasal sinuses, intolerance to acetylsalicylic acid and preparations of pyrazolone series).

From the liver and bile ducts: very rarely - Reye's syndrome (encephalopathy and acute fatty liver dystrophy with acute development of liver failure).

Overdose:

Symptoms (single dose less than 150 mg / kg - acute poisoning is considered light, 150-300 mg / kg - moderate, more than 300 mg / kg - severe): salicylism syndrome (nausea, vomiting, tinnitus, visual impairment, dizziness, severe headache, general malaise, fever - a poor prognostic sign in adults). Severe poisoning - hyperventilation of the lungs of the central genesis, respiratory alkalosis, metabolic acidosis, confused consciousness, drowsiness, collapse, convulsions, anuria, bleeding.Initially, central hyperventilation of the lungs leads to respiratory alkalosis - dyspnea, choking, cyanosis, cold sticky sweat; with increasing intoxication, paralysis of respiration and dissociation of oxidative phosphorylation, causing respiratory acidosis, increase.

In chronic overdose, the concentration in the plasma is poorly correlated with the severity of intoxication. The greatest risk of developing chronic intoxication is observed in the elderly with more than 100 mg / kg / day for several days. In children and elderly patients, the initial signs of salicylism are not always noticeable, so it is advisable to periodically determine the salicylate content in the blood: a concentration above 70 mg% indicates moderate or severe poisoning; above 100 mg% - about extremely severe, prognostically unfavorable. With moderate and severe poisoning, hospitalization is necessary.

Treatment: provocation of vomiting, the appointment of activated carbon and laxatives, constant monitoring of acid-base condition (CBS) and electrolyte balance; depending on the state of metabolism - the introduction of sodium bicarbonate,solution of sodium citrate or sodium lactate. The increase in reserve alkalinity increases the excretion of ACAS by alkalinizing urine. The alkalinization of urine is shown at a salicylate concentration above 40 mg% and is provided by intravenous infusion of sodium bicarbonate (88 mEq / in 1 L of 5% dextrose solution, at a rate of 10-15 ml / h / kg); the restoration of the volume of circulating blood (BCC) and the induction of diuresis are achieved by the introduction of sodium bicarbonate in the same doses and dilutions, which are repeated 2-3 times. Caution should be exercised in elderly patients in whom intensive fluid infusion can lead to pulmonary edema. It is not recommended the use of acetazolamide for alkalinization of urine (can cause acidosis and enhance the toxic effect of salicylates). Hemodialysis is indicated with a salicylate concentration of more than 100-130 mg%, in patients with chronic poisoning - 40 mg% and lower in the presence of indications (refractory acidosis, progressive deterioration, severe central nervous system damage, pulmonary edema and kidney failure). When swelling of the lungs - IVL with a mixture enriched with oxygen.

Interaction:

Acetylsalicylic acid increases the toxicity of methotrexate (reduces its renal clearance), valproic acid, the effects of narcotic analgesics,other non-steroidal anti-inflammatory drugs, oral hypoglycemic drugs, heparin, indirect anticoagulants, thrombolytic agents and platelet aggregation inhibitors, sulfonamides (including co-trimoxazole), triiodothyronine; reduces the effectiveness of uricosuric drugs (benzbromarone, sulfinpyrazone), antihypertensive drugs and diuretics (spironolactone, furosemide).

Glucocorticosteroids, alcohol and alcohol-containing drugs increase the damaging effect on the mucous membrane of the gastrointestinal tract, increase the risk of developing gastrointestinal bleeding.

Acetylsalicylic acid increases the concentration of digoxin, barbiturates and lithium preparations in blood plasma.

Antatsida, containing magnesium and / or aluminum hydroxide, slow down and worsen the absorption of acetylsalicylic acid.

Special instructions:

When using drugs containing acetylsalicylic acid in acute respiratory infections in children under 15 due to viral infections, there is a risk of developing Reye's syndrome (encephalopathy and acute fatty liver with acute development of liver failure).Symptoms of Reye's syndrome include prolonged vomiting, acute encephalopathy, and enlargement of the liver.

Acetylsalicylic acid reduces the excretion of uric acid from the body, which can cause an acute attack of gout in predisposed patients.

With prolonged use of the drug should periodically conduct a general blood test and analysis of feces for latent blood, monitor the functional state of the liver.

Before surgery, to reduce bleeding during surgery and in the post-operation period, you should cancel taking the drug for 5-7 days and inform the doctor.

Effect on the ability to drive transp. cf. and fur:

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration and speed of the psychomotor reaction.

Form release / dosage:

Tablets 500 mg.

Packaging:

For 20 or 30 tablets in cans of polymer complete with lids or cans of polyethylene terephthalate with the means of corking.

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

Each jar, 1, 2, 5, 10 or 20 contour mesh packages together with the instruction for use is placed in a pack of cardboard.

For 10 tablets in a contour non-cellular package of paper with a polymer coating.

It is allowed to pack 30 or 40 cans without a bundle with an equal number of instructions for use in a carton box (for hospitals).

300 or 500 contour non-jammed packages or contour mesh packages with an equal number of instructions for use are placed in a carton box (for hospitals).

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

4 years. Do not use after the expiration date.

Terms of leave from pharmacies:Without recipe

Registration number:LP-004828

Date of registration:26.04.2018

Expiration Date:26.04.2023

The owner of the registration certificate:IVANOVSKAYA Pharmaceutical Factory, OAO IVANOVSKAYA Pharmaceutical Factory, OAO Russia

Manufacturer: & nbsp

IVANOVSKAYA Pharmaceutical Factory, OAO Russia

Information update date: & nbsp28.05.2018

Illustrated instructions

Instructions

Acetylsalicylic acid (Acetylsalicylic acid)